AKN-028 is an Orally Active FLT3 Inhibitor

The activation of FMS like receptor tyrosine kinase 3 (FLT3) is a cytokine receptor that belongs to the receptor tyrosine kinase class III. Specifically, FLT3 signaling is important for the normal development of hematopoietic stem cells and progenitor cells. Besides, the FLT3 gene is one of the most common...

MYCMI-6 is a Selective Endogenous MYC:MAX Inhibitor

The MYC family of oncogenes (MYC, MYCN, and MYCL), encodes basic helix-loop-helix leucine zipper (bHLHZip) transcription factors. Through the HLHZip domain, MYC heterodimerizes with the bHLHZip protein MAX, which enables the MYC:MAX complex to bind E-box regulatory DNA elements throughout the genome. Therefore, it controls the transcription of a...

UT-34 is an Orally Active pan-Androgen Receptor Degrader (SARD)

Prostate cancer drugs targeting the androgen receptor (AR) are mainly competitive ligand-binding domain (LBD) binding antagonists. A common mechanism of drug resistance can inactivate it. Specifically, AR is a nuclear receptor that is activated by binding to any androgen. In addition, radical prostatectomy combined with gonadotropin and androgen synthetase...

TNO155 is an Orally Active WT SHP2 Inhibitor with Antineoplastic Activity

SHP2 is a non-receptor ubiquitous protein tyrosine phosphatase and has a relatively conserved structure and function. The SHP2 includes the PTP domain, two SH2 domains, and a C-terminal tail containing two phosphorylation sites. Binding of the N-SH2 domain with the PTP domain is able to inhibit SHP2 activity. N-SH2...

RBN-2397 is a Selective and Orally Active NAD+ Competitive PARP7 Inhibitor

PARP7 is a member belongs to the monoPARP family. The function of the monoPARPs is related to disease development in cancer and inflammatory conditions. As a key member of monoPARPs, PARP7 enables cancer cells to survive by evading immune detection. Additionally, many cells, especially lung cancer cells rely on...

BAY1082439 is an Orally Active and Selective Balanced PI3Kα/β/δ Inhibitor

Prostate cancer is among the most common malignancy in males. Among the various PI3K isoforms, PTEN-loss-induced prostate cancer in the genetically engineered Pten conditional knockout mouse model predominantly activates the PI3Kβ subunit. However, selective inhibition of PI3Kβ shows no significant anti-tumor efficacy in PTEN-null prostate cancer cell lines. It...

OTS514 is a Highly Potent TOPK Inhibitor with Anti-Myeloma Activity

Multiple myeloma represents a heterogeneous disease with various oncogenic mutations, chromosomal translocations, and copy number variations. The mitotic kinase T-LAK cell‐originated protein kinase/PDZ‐binding kinase ( TOPK/PBK) associates with the proliferation of tumor cells, maintenance of cancer stem cells, and poor patient prognosis in many cancers. In addition, TOPK plays...